The present invention relates broadly to the field of healthcare, and in particular, to the treatment of severe headaches in human beings. More specifically, this invention relates to compositions and methods for providing relief from the symptoms of migraine headaches and/or cluster headaches and/or headaches related to sinus congestion, in affected individuals who also have a low tolerance for aspirin due to digestive disorders.
Migraine is a particularly painful headache, which recurs and can be physically debilitating to sufferers. In many respects, cluster headaches are similar to migraine headaches, and all references herein to migraine and/or migraine headaches shall be considered as also including, and as references to, cluster headaches. There is no single cause or remedy for migraine headaches, and the incidence of migraine appears to be increasing in the general population. Although sufferers, on average, experience only one attack per month, each attack can last between four and seventy-two hours. In some cases, sufferers experience a pre-onset xe2x80x9cwarningxe2x80x9d which may indicate that a migraine is imminent, and which may be termed an xe2x80x9caura.xe2x80x9d An xe2x80x9cauraxe2x80x9d is a disruption of brain function characterized by visual disturbances like flashing lights and blurred vision. These xe2x80x9cdisruptionsxe2x80x9d occur twenty to thirty minutes before an attack. About twenty percent of migraine suffers experience xe2x80x9cauraxe2x80x9d symptoms. Other attacks can be preceded by a xe2x80x9cprodromexe2x80x9d several hours before the onset of a migraine. These xe2x80x9cprodromexe2x80x9d symptoms may include, but are not limited to, fatigue, yawning, sensory sensitivity, mood changes, and food cravings.
Prescription medications have previously been developed to alleviate the severity of migraine pain, but prescription migraine medications generally contain some type of narcotic, which, over time, may become addictive. Although over-the-counter remedies also exist, marketed under the EXCEDRIN(copyright) and ADVIL(copyright) brands, the EXCEDRIN(copyright) Migraine Formula contains aspirin, acetaminophen, and caffeine as its active ingredients, while the only active ingredient of the ADVIL(copyright) Migraine product is ibuprofen. Many migraine sufferers cannot take aspirin, due to digestive disorders, such as acid reflux disease, ulcers, and acid indigestion, and for many such sufferers, ibuprofen alone is not sufficient to lessen the pain or to reduce it to a manageable level. It would therefore be desirable to provide a non-prescription remedy which alleviates migraine symptoms in a manner not accomplished by the currently available xe2x80x9cover-the-counterxe2x80x9d remedies.
Sinus congestion (sinusitis) is also a cause of severe headaches, which can produce some of the same symptoms as migraine, such as nausea, vomiting, severe pain, and sensitivity to light, and severe sinus headache sufferers can sometimes experience xe2x80x9cauraxe2x80x9d and/or xe2x80x9cprodromexe2x80x9d symptoms as well. Current over-the-counter remedies specifically formulated to treat severe sinus headaches contain antihistamines and decongestants, in addition to analgesics. However, antihistamines provide relief only if sinusitis is caused by an allergy, and although a decongestant can be helpful, it also can worsen the symptoms if the sinusitis does not result from infection or is acute, because a decongestant will dry up the mucous membranes and can cause further impaction of the sinus cavities.
In the case of chronic sinusitis, an expectorant may be more helpful by liquefying the mucous and allowing the sinus cavities to drain, thereby relieving the pressure contributing to severe sinus headache. Expectorants are commonly used in over-the-counter medicines, but primarily in the treatment of coughs and chest congestion, not for sinus pain relief.
No currently available over-the-counter remedy provides for an expectorant combined with relief from the migraine-like symptoms of severe sinus headache, and it would therefore be desirable to provide a non-narcotic, non-prescription remedy which alleviates those symptoms, without the use of a decongestant or an antihistamine, in a manner not accomplished by the currently available over-the-counter remedies.
Recent research and clinical trials suggest that the mineral magnesium can provide some relief from migraine symptoms, at least in sufferers who have a measurable magnesium deficiency. A large percentage of the population of sufferers may indeed show this deficiency, which may contribute to migraine onset, and sufferers of severe sinus headache may exhibit this deficiency as well. Thus, an over-the-counter remedy for cluster and/or migraine headache should address potential magnesium deficiency and sensitivity to aspirin, but should also be strong enough to provide relief, and an over-the-counter remedy for severe sinus headache should address congested and impacted sinus cavities as well. The present invention is directed to meeting one or more of the above-stated desirable objectives.
The invention provides compositions, in pharmaceutically effective forms and amounts, as well as methods, for treating both migraine/cluster headaches and severe sinus headaches, in human beings in need of such treatment.
In accordance with one aspect of the invention, a migraine/cluster headache remedy is provided by combining a pain-masking analgesic (such as acetaminophen), a nonsteroidal anti-inflammatory agent (such as ibuprofen), a central nervous system stimulant (such as caffeine), and magnesium.
A feature of this aspect of the invention is that it provides pain relief through the combination of acetaminophen and ibuprofen, neither of which contains any aspirin.
Another feature of this aspect of the invention is the inclusion of the mineral magnesium as an active ingredient to remedy severe headache. This mineral ingredient advantageously addresses magnesium deficiency and its link to migraine/cluster headache cause.
In accordance with another aspect of the invention, a severe sinus headache remedy is provided by combining an expectorant (such as guaifenesin) with a pain-masking analgesic (such as acetaminophen), a nonsteroidal anti-inflammatory agent (such as ibuprofen), a central nervous system stimulant (such as caffeine), and magnesium.
A feature of this aspect of the invention, in addition to the features set forth above, is that it provides an expectorant (guaifenesin) as a means for inducing drainage of mucous secretions from the sinus passageways, without using a decongestant or antihistamine.
In accordance with a first embodiment of the invention, the combination of four active ingredients namely, acetaminophen, ibuprofen, caffeine and magnesium, in a pharmaceutically-acceptable form and in therapeutically-effective dosage, provides strong pain relief for sufferers of migraine/cluster headaches. Generally, these ingredients are utilized in the following amounts for a single dose: 100-500 mg. of acetaminophen, 100-500 mg. of ibuprofen, 25-150 mg. of caffeine and 100-500 mg. of magnesium. Preferably, the following amounts of these ingredients are used: 200-400 mg. of acetaminophen, 200-400 mg. of ibuprofen, 50-100 mg. of caffeine and 150-400 mg. of magnesium. Most preferably, the inventive composition comprises the following amounts of these ingredients: approximately 250 mg. of acetaminophen, approximately 250 mg. of ibuprofen, approximately 75 mg. of caffeine and approximately 250 mg. of magnesium.
In accordance with a second embodiment of the invention, the combination of five active ingredients, namely, guaifenesin, acetaminophen, ibuprofen, caffeine and magnesium, in a pharmaceutically-acceptable form and in a therapeutically-effective dosage, provides strong pain relief as well as sinus drainage for sufferers of severe sinus headaches. Generally, these ingredients are utilized in the following amounts for a single dose: 200-400 mg. of guaifenesin, 100-500 mg. of acetaminophen, 100-500 mg. of ibuprofen, 25-150 mg. of caffeine and 100-500 mg. of magnesium. Preferably, the following amounts of these ingredients are used: 300-400 mg. of guaifenesin, 200-400 mg. of acetaminophen, 200-400 mg. of ibuprofen, 50-100 mg. of caffeine and 150-400 mg. of magnesium. Most preferably, the inventive composition comprises the following amounts of these ingredients: approximately 400 mg. of guaifenesin, approximately 250 mg. of acetaminophen, approximately 250 mg. of ibuprofen, approximately 75 mg. of caffeine and approximately 250 mg. of magnesium.
Each embodiment of the invention further encompasses methods for treating human beings suffering from these types of headaches, comprising administering the combinations of ingredients described above together with a pharmaceutically-acceptable carrier.
Guaifenesin, acetaminophen, ibuprofen, caffeine, and magnesium are all in the public domain. The chemical name for acetaminophen is 4xe2x80x2-hydroxyacetanilide, having the empirical formula C8H9NO2. Ibuprofen is known chemically as (35)-2-(p-isobutylphenyl)propionic acid, with the formula C13H18O2, while guaifenesin has the chemical name 3-(2-methoxphenoxy)-1,2-propanediol, and has the formula C10H14O4. The empirical formula for caffeine is C8H10N4O2.
Acetaminophen, ibuprofen, and guaifenesin can all be procured in tablet form from Aceto Corporation of Lake Success, N.Y. Magnesium can be obtained easily, in either tablet or capsule form, from a number of sources including, but not limited to, Twinlab Corporation of Hauppauge, N.Y., Weider Nutrition International, Inc. of Salt Lake City, Utah (under the Schiff(copyright) brand), or even through the Internet from VitaminShoppe.com, Inc. at http://www.vitaminshoppe.com. Caffeine is available in tablet form from SmithKline Beecham of Philadelphia, Pa. It can also be isolated from tea relatively simply, in a well-known manner, as demonstrated in the experiments conducted annually as an exercise by the students in the Department of Chemistry at Okanagan University College, located in Kelowna, British Columbia, Canada. As reported (at http:www.sci.ouc.bc./chem/faculty/neeland2.html on the Internet), these experiments were modified to a micro scale, using the contents of only one tea bag, which yielded approximately 10-12 mg. of caffeine.